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INTRODUCTION

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esomeprazole (es-oh-mep-ra-zole)

Nexium

Classification

Therapeutic: antiulcer agents

Pharmacologic: proton-pump inhibitors

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Indications
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GERD/erosive esophagitis. Hypersecretory conditions, including Zollinger-Ellison syndrome. With amoxicillin and clarithromycin to eradicate Helicobacter pylori in duodenal ulcer disease or history of duodenal ulcer disease. Decrease risk of gastric ulcer during continuous NSAID therapy.

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Action
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Binds to an enzyme on gastric parietal cells in the presence of acidic gastric pH, preventing the final transport of hydrogen ions into the gastric lumen. Therapeutic Effects: Diminished accumulation of acid in the gastric lumen with lessened gastroesophageal reflux. Healing of duodenal ulcers. Decreased incidence of gastric ulcer during continuous NSAID therapy.

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Adverse Reactions/Side Effects
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CNS: headache. GI: abdominal pain, constipation, diarrhea, dry mouth, flatulence, nausea.

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PHYSICAL THERAPY IMPLICATIONS

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Examination and Evaluation
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  • Monitor improvements in GI symptoms (gastritis, heartburn, and so forth) to help determine if drug therapy is successful.

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Interventions
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  • In cases of NSAID-induced gastritis, implement appropriate manual therapy techniques, physical agents, and therapeutic exercises to reduce pain and decrease the need for aspirin and other NSAIDs.

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Patient/Client-Related Instruction
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  • Advise patient to avoid alcohol and foods that may cause an increase in GI irritation.

  • Instruct patient to report bothersome or prolonged side effects, including headache or GI effects (nausea, constipation, diarrhea flatulence, abdominal pain, dry mouth).

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Pharmacokinetics
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Absorption: 90% absorbed following oral administration; food decreases absorption.

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Distribution: Unknown.

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Protein Binding: 97%.

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Metabolism and Excretion: Extensively metabolized by the liver (cytochrome P450 [CY P450] system, primarily CYP2C19 isoenzyme); <1% excreted unchanged in urine.

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Half-life: 1.0–1.5 hr.

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TIME/ACTION PROFILE (blood levels*)

ROUTE ONSET PEAK DURATION
PO rapid 1.6 hr 24 hr
IV rapid end of infusion 24 hr

*Resolution of symptoms takes 5–8 days.

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Contraindications/Precautions
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Contraindicated in: Hypersensitivity; OB: Lactation (not recommended).

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Use Cautiously in: Severe hepatic impairment (daily dose should not exceed 20 mg); Geri: Increased risk of hip fractures in patients using high doses for >1 year; OB: Pregnancy (use only if clearly needed); Pedi: Children <1 yr (safety not established).

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Interactions
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Drug-Drug: May ↓ absorption of drugs requiring acid pH, including ketoconazole, itraconazole, atazanavir, ampicillin, iron salts, and digoxin. May ↑ risk of bleeding with warfarin (monitor INR and PT).

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Route/Dosage
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Gastroesophageal Reflux Disease
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PO (Adults): Healing of erosive esophagitis—20 or 40 mg once daily for 4–8 wk; maintenance of healing of erosive esophagitis—20 mg once daily; symptomatic GERD—20 mg once daily for 4 wk (additional 4 ...

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